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Recent developments on (−)-colchicine derivatives: Synthesis and structure-activity relationship

Ghawanmeh, Abdullah A. and Al-Bajalan, Hussein M. and Mackeen, Mukram Mohamed and Alali, Feras Q. and K. F., Chong (2019) Recent developments on (−)-colchicine derivatives: Synthesis and structure-activity relationship. European Journal of Medicinal Chemistry, 185 (111788). pp. 1-16. ISSN 0223-5234

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Abstract

(−)-Colchicine, an anti-microtubulin polymerization agent, is a valuable medication and the drug of choice for gout, Behçet’s disease and familial Mediterranean fever. It has a narrow therapeutic index due to its high toxicity towards normal cells. Nonetheless, numerous (−)-colchicine derivatives have been synthesized and studied for their structure-activity relationship and preferential toxicity. Different functional groups such as amides, thioamides, N-arylurea and 8,12-diene cyclic have been incorporated into (−)-colchicine, resulting in derivatives (with moieties) that include electron-withdrawing and electron-donating groups. This review article focuses on recent developments in the chemical synthesis of (−)-colchicine derivatives, the substituents used, the functional groups linked to the substituents, the moieties and biological studies. Moreover, the current classification of derivatives based on the (−)-colchicine rings, namely ring A, B, and C (−)-colchicine derivatives, is discussed. This work demonstrates and summarizes the significance of (−)-colchicine derivatives in the biological field, and discusses their promising therapeutics for the future.

Item Type: Article
Additional Information: Indexed byScopus
Uncontrolled Keywords: (−)-Colchicine; (−)-Colchicine derivatives; Structure-activity relationship
Subjects: T Technology > TP Chemical technology
Faculty/Division: Faculty of Industrial Sciences And Technology
Institute of Postgraduate Studies
Depositing User: Mrs Norsaini Abdul Samat
Date Deposited: 06 Dec 2019 04:07
Last Modified: 06 Dec 2019 04:07
URI: http://umpir.ump.edu.my/id/eprint/26482
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